JP2015520753A5 - - Google Patents
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- JP2015520753A5 JP2015520753A5 JP2015512120A JP2015512120A JP2015520753A5 JP 2015520753 A5 JP2015520753 A5 JP 2015520753A5 JP 2015512120 A JP2015512120 A JP 2015512120A JP 2015512120 A JP2015512120 A JP 2015512120A JP 2015520753 A5 JP2015520753 A5 JP 2015520753A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- treating
- pharmaceutical composition
- composition according
- compound according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 63
- 201000011510 cancer Diseases 0.000 claims description 59
- 230000002401 inhibitory effect Effects 0.000 claims description 29
- 239000008194 pharmaceutical composition Substances 0.000 claims description 26
- 239000003112 inhibitor Substances 0.000 claims description 20
- 101710015564 CHEK1 Proteins 0.000 claims description 16
- 102100019702 CHEK1 Human genes 0.000 claims description 16
- 239000003795 chemical substances by application Substances 0.000 claims description 14
- 102100015262 MYC Human genes 0.000 claims description 13
- 206010029260 Neuroblastoma Diseases 0.000 claims description 12
- 230000002018 overexpression Effects 0.000 claims description 12
- 210000004027 cells Anatomy 0.000 claims description 9
- 206010006187 Breast cancer Diseases 0.000 claims description 8
- 231100000277 DNA damage Toxicity 0.000 claims description 8
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 8
- 206010025650 Malignant melanoma Diseases 0.000 claims description 8
- 108091008108 Myc family Proteins 0.000 claims description 8
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims description 8
- 102000005497 Thymidylate Synthase Human genes 0.000 claims description 8
- 108010067449 Thymidylate Synthase Proteins 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 8
- 201000005202 lung cancer Diseases 0.000 claims description 8
- 201000001441 melanoma Diseases 0.000 claims description 8
- 201000002528 pancreatic cancer Diseases 0.000 claims description 8
- 230000011664 signaling Effects 0.000 claims description 8
- 206010033128 Ovarian cancer Diseases 0.000 claims description 7
- 201000011231 colorectal cancer Diseases 0.000 claims description 7
- 102100018882 MYCN Human genes 0.000 claims description 6
- 108010010748 N-Myc Proto-Oncogene Protein Proteins 0.000 claims description 6
- -1 hydrate Substances 0.000 claims description 6
- 238000000338 in vitro Methods 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000011780 sodium chloride Substances 0.000 claims description 6
- 239000012453 solvate Substances 0.000 claims description 6
- 208000003950 B-Cell Lymphoma Diseases 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 102000003915 DNA Topoisomerases Human genes 0.000 claims description 4
- 108090000323 DNA Topoisomerases Proteins 0.000 claims description 4
- 206010017758 Gastric cancer Diseases 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- 206010020243 Hodgkin's disease Diseases 0.000 claims description 4
- 206010024324 Leukaemias Diseases 0.000 claims description 4
- 210000004688 Microtubules Anatomy 0.000 claims description 4
- 102000028664 Microtubules Human genes 0.000 claims description 4
- 108091022031 Microtubules Proteins 0.000 claims description 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 206010039491 Sarcoma Diseases 0.000 claims description 4
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 claims description 4
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 claims description 4
- 230000004913 activation Effects 0.000 claims description 4
- 201000005188 adrenal gland cancer Diseases 0.000 claims description 4
- 230000001668 ameliorated Effects 0.000 claims description 4
- 230000000340 anti-metabolite Effects 0.000 claims description 4
- 239000002256 antimetabolite Substances 0.000 claims description 4
- 229920003013 deoxyribonucleic acid Polymers 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 201000004101 esophageal cancer Diseases 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 201000000349 mediastinal cancer Diseases 0.000 claims description 4
- 230000001404 mediated Effects 0.000 claims description 4
- 230000000394 mitotic Effects 0.000 claims description 4
- 230000017205 mitotic cell cycle checkpoint Effects 0.000 claims description 4
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 4
- 201000008968 osteosarcoma Diseases 0.000 claims description 4
- 230000002062 proliferating Effects 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 201000002510 thyroid cancer Diseases 0.000 claims description 4
- 102000004190 Enzymes Human genes 0.000 claims description 3
- 108090000790 Enzymes Proteins 0.000 claims description 3
- 206010027476 Metastasis Diseases 0.000 claims description 3
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims description 3
- 201000009036 biliary tract cancer Diseases 0.000 claims description 3
- 230000002950 deficient Effects 0.000 claims description 3
- 201000011682 nervous system cancer Diseases 0.000 claims description 3
- 201000002314 small intestine cancer Diseases 0.000 claims description 3
- 238000002560 therapeutic procedure Methods 0.000 claims description 3
- 230000006907 apoptotic process Effects 0.000 claims description 2
- 230000022131 cell cycle Effects 0.000 claims description 2
- 230000036210 malignancy Effects 0.000 claims description 2
- 230000001737 promoting Effects 0.000 claims description 2
- 206010059512 Apoptosis Diseases 0.000 claims 1
- 210000001072 Colon Anatomy 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010038038 Rectal cancer Diseases 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 description 21
- 238000004519 manufacturing process Methods 0.000 description 17
- 229940079593 drugs Drugs 0.000 description 4
- 230000000051 modifying Effects 0.000 description 3
- 206010004593 Bile duct cancer Diseases 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 201000011061 large intestine cancer Diseases 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006011 modification reaction Methods 0.000 description 1
- 210000000653 nervous system Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261647200P | 2012-05-15 | 2012-05-15 | |
| US61/647,200 | 2012-05-15 | ||
| PCT/GB2013/051233 WO2013171470A1 (en) | 2012-05-15 | 2013-05-14 | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016201383A Division JP6362652B2 (ja) | 2012-05-15 | 2016-10-13 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015520753A JP2015520753A (ja) | 2015-07-23 |
| JP2015520753A5 true JP2015520753A5 (id) | 2016-04-14 |
| JP6027230B2 JP6027230B2 (ja) | 2016-11-16 |
Family
ID=48468659
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512120A Active JP6027230B2 (ja) | 2012-05-15 | 2013-05-14 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
| JP2016201383A Active JP6362652B2 (ja) | 2012-05-15 | 2016-10-13 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016201383A Active JP6362652B2 (ja) | 2012-05-15 | 2016-10-13 | ５−［［４−［［モルホリン−２−イル］メチルアミノ］−５−（トリフルオロメチル）−２−ピリジル］アミノ］ピラジン−２−カルボニトリルおよびその治療上の使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US9663503B2 (id) |
| EP (2) | EP3210980B1 (id) |
| JP (2) | JP6027230B2 (id) |
| KR (6) | KR102090792B1 (id) |
| CN (2) | CN106279142B (id) |
| AU (2) | AU2013261605B2 (id) |
| BR (1) | BR112014026801B1 (id) |
| CA (1) | CA2870837C (id) |
| DK (1) | DK2855448T3 (id) |
| ES (2) | ES2981584T3 (id) |
| HK (2) | HK1203529A1 (id) |
| IL (1) | IL235133A (id) |
| IN (1) | IN2014DN09221A (id) |
| MX (1) | MX358819B (id) |
| NZ (1) | NZ702050A (id) |
| PL (1) | PL2855448T3 (id) |
| RU (1) | RU2659786C2 (id) |
| SG (1) | SG11201407238VA (id) |
| WO (1) | WO2013171470A1 (id) |
| ZA (1) | ZA201408452B (id) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013068755A1 (en) | 2011-11-09 | 2013-05-16 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| CA2870837C (en) | 2012-05-15 | 2022-05-10 | Cancer Research Technology Limited | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
| LT3418281T (lt) | 2012-12-07 | 2021-01-11 | Vertex Pharmaceuticals Inc. | Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| PT3077397T (pt) | 2013-12-06 | 2020-01-22 | Vertex Pharma | Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo |
| RS60013B1 (sr) | 2014-06-05 | 2020-04-30 | Vertex Pharma | Radioaktivno obeleženi derivati jedinjenja 2-amino-6-fluoro-n-[5-fluoropiridin-3-il]pirazolo[1,5-a]pirimidin-3-karboksamida, korisnog kao inhibitora atr kinaze, dobijanje pomenutog jedinjenja i njegovi različiti čvrsti oblici |
| CA2950780C (en) * | 2014-06-17 | 2023-05-16 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of chk1 and atr inhibitors |
| AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| WO2018094325A1 (en) * | 2016-11-18 | 2018-05-24 | The Trustees Of Columbia University In The City Of New York | Therapeutic modulation of oncogenes by pharmacologic top2 targeting for cancer |
| WO2018183891A1 (en) * | 2017-03-31 | 2018-10-04 | Cascadian Therapeutics | Combinations of chk1- and wee1 - inhibitors |
| JP7273791B2 (ja) * | 2017-04-10 | 2023-05-15 | シエラ オンコロジー， インコーポレイテッド | 腫瘍成長を阻害するＣＨＫ１（ＳＲＡ７３７）／ＰＡＲＰｉ組み合わせ方法 |
| WO2018191299A1 (en) * | 2017-04-10 | 2018-10-18 | Sierra Oncology, Inc. | Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth |
| CA3065803A1 (en) * | 2017-06-01 | 2018-12-06 | Sierra Oncology, Inc. | Biomarkers and patient selection strategies |
| CN107266897B (zh) * | 2017-08-04 | 2019-05-14 | 上海跃贝新材料科技股份有限公司 | 一种低粘度矿物增强pc/pet合金材料及其制备方法 |
| WO2019165458A1 (en) * | 2018-02-26 | 2019-08-29 | Sierra Oncology, Inc. | Methods of treatment of cancer comprising chk1 inhibitors |
| WO2020154608A1 (en) * | 2019-01-25 | 2020-07-30 | Numedii, Inc. | Method for treating idiopathic pulmonary fibrosis |
| CA3135165A1 (en) * | 2019-03-28 | 2020-10-01 | Sierra Oncology, Inc. | Methods of treating cancer with chk1 inhibitors |
| MX2021013905A (es) * | 2019-05-14 | 2022-05-18 | Sierra Oncology Inc | Métodos de tratamiento del cáncer mediante el uso de inhibidores de chk1. |
| CN110872277B (zh) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-取代芳环-2-氨基嘧啶类化合物及用途 |
| CN110680928B (zh) * | 2019-12-06 | 2020-04-28 | 深圳前海港影生物科技有限公司 | 抑制黑色素合成的偶联物及其在药品和化妆品中的应用 |
| CN110684083B (zh) * | 2019-12-06 | 2020-05-15 | 北京诺赛启研再生医学研究院有限公司 | 抑制黑色素合成的偶联物ii及其在药品和化妆品中的应用 |
| TW202204348A (zh) * | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Ｃｈｋ１抑制劑之合成方法 |
| EP4387959A1 (en) * | 2021-08-17 | 2024-06-26 | GlaxoSmithKline Intellectual Property (No.3) Limited | Preparation of a p2x3 antagonist |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773778A (en) | 1972-01-24 | 1973-11-20 | Squibb & Sons Inc | Sulfur derivatives of pyrazolo (3,4-b)pyridines |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| CA2224435C (en) | 1995-07-06 | 2008-08-05 | Novartis Ag | Pyrrolopyrimidines and processes for the preparation thereof |
| EP1435947B1 (en) | 2001-10-19 | 2007-08-15 | Ortho-McNeil Pharmaceutical, Inc. | 2-phenyl benzimidazoles and imidazo-¬4,5|-pyridines as cds1/chk2-inhibitors and adjuvants to chemotherapy or radiation therapy in the treatment of cancer |
| AU2002334217B2 (en) | 2001-10-26 | 2008-07-03 | Aventis Pharmaceuticals Inc. | Benzimidazoles and analogues and their use as protein kinases inhibitors |
| JP2005515173A (ja) | 2001-10-31 | 2005-05-26 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | ピリミド［４，５−ｂ］インドール誘導体 |
| AU2003234464B2 (en) | 2002-05-03 | 2009-06-04 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| WO2003101444A1 (en) | 2002-05-29 | 2003-12-11 | Millennium Pharmaceuticals, Inc. | Diarylurea compounds and derivatives as chk-1 inhibitors for the treatment of cancer |
| CN1860118A (zh) | 2003-07-29 | 2006-11-08 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| JP4758349B2 (ja) | 2003-10-08 | 2011-08-24 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| US7326712B2 (en) | 2003-10-14 | 2008-02-05 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Substituted tricyclic compounds as protein kinase inhibitors |
| US7691866B2 (en) | 2003-10-16 | 2010-04-06 | Novartis Vaccines And Diagnostics, Inc. | 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines and methods of their use as inhibitors of Raf kinase |
| US7163939B2 (en) | 2003-11-05 | 2007-01-16 | Abbott Laboratories | Macrocyclic kinase inhibitors |
| US20050096324A1 (en) | 2003-11-05 | 2005-05-05 | Zhi-Fu Tao | Macrocyclic kinase inhibitors |
| CA2561831A1 (en) | 2004-04-13 | 2005-12-22 | Icagen, Inc. | Polycyclic pyrazines as potassium ion channel modulators |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| KR20080020602A (ko) | 2005-04-28 | 2008-03-05 | 수퍼젠, 인크. | 단백질 키나아제 저해제 |
| AU2006264043B2 (en) | 2005-06-28 | 2012-04-26 | Sanofi-Aventis | Isoquinoline derivatives as inhibitors of Rho-kinase |
| PE20070427A1 (es) | 2005-08-30 | 2007-04-21 | Novartis Ag | Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas |
| CN101321760A (zh) | 2005-10-06 | 2008-12-10 | 先灵公司 | 作为蛋白激酶抑制剂的吡唑并嘧啶 |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| GB0616747D0 (en) * | 2006-08-24 | 2006-10-04 | Astrazeneca Ab | Novel compounds |
| CN101611012B (zh) | 2006-12-27 | 2012-11-14 | 塞诺菲-安万特股份有限公司 | 环烷基胺取代的异喹啉衍生物 |
| CA2681015C (en) | 2007-03-16 | 2016-06-21 | The Scripps Research Institute | Inhibitors of focal adhesion kinase |
| WO2008117050A1 (en) | 2007-03-27 | 2008-10-02 | Astrazeneca Ab | Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer |
| EP2170886A1 (en) | 2007-07-02 | 2010-04-07 | Cancer Research Technology Limited | 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors |
| GB0719644D0 (en) | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB0803018D0 (en) | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| WO2013068755A1 (en) | 2011-11-09 | 2013-05-16 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| CA2870837C (en) | 2012-05-15 | 2022-05-10 | Cancer Research Technology Limited | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
-
2013
- 2013-05-14 CA CA2870837A patent/CA2870837C/en active Active
- 2013-05-14 RU RU2014147105A patent/RU2659786C2/ru active
- 2013-05-14 NZ NZ702050A patent/NZ702050A/en unknown
- 2013-05-14 EP EP17152400.2A patent/EP3210980B1/en active Active
- 2013-05-14 KR KR1020147031572A patent/KR102090792B1/ko active IP Right Grant
- 2013-05-14 DK DK13723910.9T patent/DK2855448T3/en active
- 2013-05-14 KR KR1020207007411A patent/KR102246265B1/ko active IP Right Grant
- 2013-05-14 CN CN201610652725.8A patent/CN106279142B/zh active Active
- 2013-05-14 ES ES17152400T patent/ES2981584T3/es active Active
- 2013-05-14 EP EP13723910.9A patent/EP2855448B1/en active Active
- 2013-05-14 IN IN9221DEN2014 patent/IN2014DN09221A/en unknown
- 2013-05-14 BR BR112014026801-0A patent/BR112014026801B1/pt active IP Right Grant
- 2013-05-14 CN CN201380025541.3A patent/CN104302635B/zh active Active
- 2013-05-14 US US14/396,338 patent/US9663503B2/en active Active
- 2013-05-14 ES ES13723910.9T patent/ES2624307T3/es active Active
- 2013-05-14 PL PL13723910T patent/PL2855448T3/pl unknown
- 2013-05-14 MX MX2014012881A patent/MX358819B/es active IP Right Grant
- 2013-05-14 KR KR1020217041302A patent/KR20210156333A/ko not_active Application Discontinuation
- 2013-05-14 KR KR1020217012299A patent/KR102341637B1/ko active IP Right Grant
- 2013-05-14 JP JP2015512120A patent/JP6027230B2/ja active Active
- 2013-05-14 WO PCT/GB2013/051233 patent/WO2013171470A1/en active Application Filing
- 2013-05-14 KR KR1020227037439A patent/KR102635954B1/ko active IP Right Grant
- 2013-05-14 SG SG11201407238VA patent/SG11201407238VA/en unknown
- 2013-05-14 AU AU2013261605A patent/AU2013261605B2/en active Active
- 2013-05-14 KR KR1020247004407A patent/KR20240023685A/ko active Application Filing
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2014
- 2014-10-19 IL IL235133A patent/IL235133A/en active IP Right Grant
- 2014-11-18 ZA ZA2014/08452A patent/ZA201408452B/en unknown
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2015
- 2015-04-28 HK HK15104108.4A patent/HK1203529A1/xx unknown
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2016
- 2016-10-13 JP JP2016201383A patent/JP6362652B2/ja active Active
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2017
- 2017-05-04 US US15/587,270 patent/US10259806B2/en active Active
- 2017-11-28 AU AU2017268508A patent/AU2017268508C1/en active Active
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2018
- 2018-02-27 HK HK18102805.1A patent/HK1243408A1/zh unknown
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2020
- 2020-12-17 US US17/124,606 patent/US11787792B2/en active Active
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